WO2011147280A1 - 一种恩诺沙星注射液及其制备方法 - Google Patents

一种恩诺沙星注射液及其制备方法 Download PDF

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Publication number
WO2011147280A1
WO2011147280A1 PCT/CN2011/074426 CN2011074426W WO2011147280A1 WO 2011147280 A1 WO2011147280 A1 WO 2011147280A1 CN 2011074426 W CN2011074426 W CN 2011074426W WO 2011147280 A1 WO2011147280 A1 WO 2011147280A1
Authority
WO
WIPO (PCT)
Prior art keywords
enrofloxacin
injection
chelating agent
solution
sodium
Prior art date
Application number
PCT/CN2011/074426
Other languages
English (en)
French (fr)
Chinese (zh)
Inventor
董惠峰
Original Assignee
鼎正动物药业(天津)有限公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 鼎正动物药业(天津)有限公司 filed Critical 鼎正动物药业(天津)有限公司
Priority to KR1020127021886A priority Critical patent/KR20130080422A/ko
Priority to AU2011257785A priority patent/AU2011257785A1/en
Publication of WO2011147280A1 publication Critical patent/WO2011147280A1/zh

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents

Definitions

  • the invention relates to an antibacterial medicine for preventing and controlling aquatic diseases of livestock and poultry, in particular to an enrofloxacin injection and a preparation method thereof. Background technique
  • Enrofloxacin (English name: Enrofloxacin), its chemical formula is 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-ethyl-1-piperazinyl)- 3-quinolinecarboxylic acid (English name: 1, 4-dihydro-l-cyclopropyl-7- (4-ethyl-l-piperazinyl) -6 ⁇ f luoro-4-oxo-3-quinol i
  • quinolone antibacterial drugs is a representative of a new generation of quinolone antibacterial drugs. It is a special new drug for the prevention and control of aquatic diseases in livestock and poultry. It not only retains the characteristics of broad-spectrum, high-efficiency, low toxicity, good absorption and convenient administration of quinolones, but also various Various infections caused by bacteria have significant effects, especially for various mycoplasma. The killing power of various mycoplasma is significantly higher than other drugs of quinolones and various drugs such as tylosin and tyrosin which have been used for many years. However, since enrofloxacin has a very strong bitter taste, when used as an oral dosage form, the tolerance of the animal is very low, so it is usually administered in the form of an injection in clinical use.
  • Enrofloxacin is very soluble in water and dissolves in alkaline solvents, so the commonly used injection is an alkaline aqueous solution of enrofloxacin, the alkaline aqueous solution is an aqueous solution of sodium hydroxide, but enrofloxacin is in an alkaline aqueous solution.
  • the solubility in the solution was 10%, and the excess portion precipitated in a crystalline form.
  • the object of the present invention is to overcome the deficiencies of the prior art, and to provide an enrofloxacin injection having a neutral pH and no stimulation to an animal, wherein the content of enrofloxacin in the injection is 10 to 20%. It greatly increases the therapeutic effect of single administration, and the prepared enrofloxacin injection has stable traits and long-term storage without crystallization, which is a kind of injection with good therapeutic effect and no stimuli.
  • the espresso agent is 0. 1 ⁇ 0. 5 parts.
  • the chelating agent is 0. 1 ⁇ 0. 5 parts.
  • the enrofloxacin accounts for 10 to 20% of the total weight of the solution.
  • the antioxidant is sodium thiosulfate or sodium hydrogen sulfite.
  • the chelating agent is EDTA.
  • the invention also provides a preparation method of enrofloxacin injection, the method comprising the following steps:
  • the sterilizing treatment is performed by using a 45.
  • the concentration of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of the aqueous solution of The acidifying agent in the step (3) is one or two or three kinds of lactic acid, sodium butyrate or arginine.
  • the antioxidant in step (4) is sodium thiosulfate or
  • the enrofloxacin injection prepared by the present invention is added with one or two or three kinds of lactic acid, sodium butyrate or arginine, and finally the pH of the injection is made.
  • Neutral which is not irritating when the animal is injected, and increases the amount of enrofloxacin in the injection to 20%, greatly increasing the therapeutic effect of a single administration, and simultaneously preparing the enrofloxacin injection. It has stable liquid properties and long-term storage without crystal precipitation. It is a kind of injection with good therapeutic effect and no stimulation.
  • the present invention the singularity of the singularity of the singularity of the singularity of the singularity of the singularity of the singularity of the singularity of the singularity of the singularity. 5 ⁇
  • the chelating agent 0. 1 ⁇ 0. 5 parts. Enrofloxacin accounts for 10 to 20% of the total weight of the solution.
  • the antioxidant is sodium thiosulfate or sodium hydrogen sulfite.
  • the chelating agent is EDTA (Ethyl ene Diamine Tetraacet i c Ac i d).
  • a method for preparing enrofloxacin injection comprises the following steps:
  • Step (5) After completion, the volume is adjusted to 100 ml with purified water, and the solution after constant volume is filtered through a microporous membrane of 0. 45 um;
  • the enrofloxacin injection was tested to be neutral, and the enzyfloxacin content of the active ingredient in the solution injection was 20% of the total weight of the injection solution.
  • a method for preparing enrofloxacin injection comprises the following steps:
  • Step (5) After completion, the volume is adjusted to 100 ml with purified water, and the solution after constant volume is filtered through a microporous membrane of 0. 45 um;
  • the enrofloxacin injection was tested to be neutral, and the enolfloxacin content of the active ingredient in the solution was
  • a method for preparing enrofloxacin injection comprises the following steps:
  • Step (5) After completion, the volume is adjusted to 100 ml with purified water, and the solution after constant volume is filtered through a microporous membrane of 0. 45 um;
  • the enrofloxacin injection was tested to be neutral, and the enolfloxacin content of the active ingredient in the solution was
  • a method for preparing enrofloxacin injection comprises the following steps:
  • Step (5) After completion, the volume is adjusted to 100 ml with purified water, and the solution after constant volume is filtered through a microporous membrane of 0. 45 um;
  • the enrofloxacin injection was tested to be neutral, and the enzyfloxacin content of the active ingredient in the solution was 18%.
  • the enrofloxacin injection prepared by the present invention has stable composition and no precipitation during long-term storage.
  • the enrofloxacin injection prepared by the present invention is not irritating to the animal, and the animal has no uncomfortable reaction after the administration.
  • Table 3 Test results of therapeutic effect of chicken artificially infected Escherichia coli As can be seen from Table 3, the enrofloxacin injection prepared by the present invention has good curative effect and high cure rate.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Organic Chemistry (AREA)
  • Dermatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
PCT/CN2011/074426 2010-05-22 2011-05-20 一种恩诺沙星注射液及其制备方法 WO2011147280A1 (zh)

Priority Applications (2)

Application Number Priority Date Filing Date Title
KR1020127021886A KR20130080422A (ko) 2010-05-22 2011-05-20 엔로플록사신의 주사제 및 그의 제조방법
AU2011257785A AU2011257785A1 (en) 2010-05-22 2011-05-20 Injection of enrofloxacin and producing method thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201010179923.X 2010-05-22
CN201010179923XA CN101810569B (zh) 2010-05-22 2010-05-22 一种恩诺沙星注射液及其制备方法

Publications (1)

Publication Number Publication Date
WO2011147280A1 true WO2011147280A1 (zh) 2011-12-01

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Country Status (4)

Country Link
KR (1) KR20130080422A (ko)
CN (1) CN101810569B (ko)
AU (2) AU2011101749A4 (ko)
WO (1) WO2011147280A1 (ko)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101810569B (zh) * 2010-05-22 2011-09-21 鼎正动物药业(天津)有限公司 一种恩诺沙星注射液及其制备方法
CN102772359A (zh) * 2012-08-02 2012-11-14 挑战(天津)动物药业有限公司 一种恩诺沙星注射液及其制备方法
CN104606671B (zh) * 2014-12-30 2017-01-18 天津市中升挑战生物科技有限公司 一种复方溶菌酶恩诺沙星注射制剂
CN104586757A (zh) * 2015-01-08 2015-05-06 邳州正康生物技术有限公司 一种兽用恩诺沙星注射液及其制备方法
CN107095848A (zh) * 2017-07-01 2017-08-29 山东中牧兽药有限公司 一种恩诺沙星注射液及其制备方法
CN112174888B (zh) * 2019-07-04 2022-10-14 天津市中升挑战生物科技有限公司 一种恩诺沙星单晶型物及其制备方法
CN111973553A (zh) * 2020-09-03 2020-11-24 江西省科达动物药业有限公司 一种高稳定性的恩诺沙星注射液及其制备方法
CN117530922B (zh) * 2024-01-09 2024-04-26 中国农业大学 一种兽用高稳定性复方注射液及其制备方法和应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1177300A (zh) * 1995-01-13 1998-03-25 拜尔公司 恩氟沙星注射液或输液
CN101400351A (zh) * 2006-03-08 2009-04-01 拜尔动物保健有限责任公司 含氟喹诺酮类化合物的药物制剂
CN101810569A (zh) * 2010-05-22 2010-08-25 鼎正动物药业(天津)有限公司 一种恩诺沙星注射液及其制备方法

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CN1288725A (zh) * 2000-06-30 2001-03-28 程广亚 畜禽注射液及其系列产品的制备方法
ES2315123B1 (es) * 2006-09-25 2009-12-30 Divasa-Farmavic, S.A. Composiciones farmaceuticas estables de tetraciclinas en solucion, procedimiento para su obtencion y sus usos.
CN101301291B (zh) * 2008-04-11 2010-09-01 天津生机集团股份有限公司 兽用复方恩诺沙星注射液及其制备方法
CN101347432B (zh) * 2008-09-05 2011-06-22 郑州后羿制药有限公司 一种畜禽用长效恩诺沙星注射液及其制备方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1177300A (zh) * 1995-01-13 1998-03-25 拜尔公司 恩氟沙星注射液或输液
CN101400351A (zh) * 2006-03-08 2009-04-01 拜尔动物保健有限责任公司 含氟喹诺酮类化合物的药物制剂
CN101810569A (zh) * 2010-05-22 2010-08-25 鼎正动物药业(天津)有限公司 一种恩诺沙星注射液及其制备方法

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Publication number Publication date
CN101810569B (zh) 2011-09-21
AU2011257785A1 (en) 2012-08-30
AU2011101749A4 (en) 2015-02-05
KR20130080422A (ko) 2013-07-12
CN101810569A (zh) 2010-08-25

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